Cycloartane triterpenoids are widely existed in the plants, in which C-9 and C-19 form a three-membered ring to form a special type of tetracyclic triterpenoid. These compounds have complex structures and diverse biological activities. The literature reports that they have anti-tumor activities, anti-viral activities, antibacterial and anti-inflammatory activities, immunomodulatory activities, cardiovascular effects, and protective effects on liver damage (TIAN Ze et al., Review of Bioactivities of Natural Cycloartane Triterpenoids, China Journal of Chinese Materia, 2006, 31(8): 626-629). The natural products of typical cycloartane triterpenoids are: for example, Cycloastragenol (derived from Radix Astragali), Astragaloside (derived from Radix Astragali), Cimigenol (derived from rhizoma cimicifugae), Oryzanol (derived from rice bran oil), Huangyangning (Cyclovirobuxin A-D, derived from Buxus sempervirens), and Cyclobuxine D, whose structures are shown as follows:

Among them, the research on astragaloside as a representative drug is a particular hotspot, and the development of its injection for angina pectoris is in the clinical trial stage. The Huangyangning tablet as Chinese patent medicine is included in Chinese Pharmacopoeia for the treatment of thoracic obstruction and cardiodynia, knotted pulse, coronary heart disease, and arrhythmia caused by stagnation of blood stasis. Oryzanol injection is used for autonomic nerve dysfunction, premenstrual tension syndrome, menopausal syndrome, and primary dysmenorrhea.
The structural modifications on steroidal drugs with tetracyclic triterpenoid structure characteristics exist throughout the history of drug development, in which the structural modifications and developments of glucocorticoid anti-inflammatory drugs are the most well-known. From prednisone to hydrocortisone, prednisolone, dexamethasone, and various water-soluble and fat-soluble prodrugs, every tiny structural change has brought about a significant increase in clinical application value. There have been increasing attentions paid to the research on cycloartane natural products also as tetracyclic triterpenoids to increase the clinical application value by improving pharmacokinetic characteristics, enhancing the pharmacological efficacy, and reducing toxic and side effects through structural modifications.
Cardiovascular and/or cerebrovascular diseases, a type of common disease that threatens humans especially middle-aged and old people who are over 50 years old, are characterized in high prevalence, high disability, and high mortality. Even if the most advanced and perfect treatment at present is applied, more than 50% of the survivors of cardiovascular and/or cerebrovascular accidents cannot completely take care of themselves. The number of people who die of cardiovascular and/or cerebrovascular diseases every year in the world is as high as 15 millions, ranking the first in all causes of death. The China National Cardiovascular Disease Center recently published the “China Cardiovascular Disease Report 2015.” This report shows that 2 out of every 5 deaths in China died of cardiovascular disease. Cardiovascular mortality is still the leading cause in death from disease, higher than cancer and other diseases. According to the report, in 2014, the mortality of cardiovascular disease in urban areas of China was 261.99/100,000 persons, wherein the mortality of heart disease was 136.21/100,000 persons, and the mortality of cerebrovascular disease was 125.78/100,000 persons (52.25/10,000 persons for cerebral hemorrhage, and 41.99/100,000 persons for cerebral infarction).
Therefore, it is quite necessary to develop a drug for the remarkable prevention and treatment of cardiovascular and/or cerebrovascular diseases. Said drug should have good drug absorption characteristics, facilitate long-term oral administration or first-aid administration, and especially have excellent pharmacological activities for prevention or treatment as well as favorable safety and therapeutic window.